A selective inhibitor of p38α MAPK (IC50 = 10 nM) that blocks IL-1β and TNF-α release in whole blood in vitro (IC50s = 150 and 180 nM

VX-745 – 5 mg

Brand:
Cayman
CAS:
209410-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.{29195} It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.{29195} VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.{21533}  

 

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Description

A selective inhibitor of p38α MAPK (IC50 = 10 nM) that blocks IL-1β and TNF-α release in whole blood in vitro (IC50s = 150 and 180 nM, respectively)

Formal name: 5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one

Synonyms: 

Molecular weight: 436.3

CAS: 209410-46-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|p38 MAPK Signaling||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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